scholarly journals Anticancer agents from Solanum Surattense

2020 ◽  
Vol 1 (1) ◽  
pp. 16-21
Author(s):  
Mahreen Mukhtar ◽  
Saima Khan ◽  
Naheed Riaz ◽  
Muhammad Imran Tousif ◽  
Mamona Nazir ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Spectroscopic Data ◽  
Methanolic Extract ◽  
Cancer Cell Line ◽  
2D Nmr ◽  
Solanum Surattense ◽  
Ic50 Value ◽  
Nmr Techniques ◽  
Nih 3T3

Two steroids glycosides solamargine (1) and dioscine (2) were isolated from methanolic extract of Solanum surattense and evaluated for their anticancer activity. The structure of the isolated compounds was identified through 1D and 2D NMR techniques, mass spectrometry and in comparison, with the literature values of their spectroscopic data. Both compounds showed the excellent anticancer activity against NIH-3T3 fibroblast cancer cell line with IC50 value of 7.55±1.5 and 3.3±1.9µg/ml respectively which were comparable with control Cyclohexamide which showed the IC50 value of 0.8± 0.2 µg/ml.

Anticancer Evaluation and Docking Study of New Bifunctional Phthalazine Derivatives

2018 ◽  
Vol 15 (3) ◽  
pp. 414-422 ◽  
Author(s):  
Marwa G. El-Gazzar ◽  
Hala M. Aly
Keyword(s):  
Anticancer Activity ◽  
Cell Line ◽  
Anticancer Agents ◽  
Active Site ◽  
Cancer Cell Line ◽  
Docking Study ◽  
Quinazoline Derivative ◽  
Spectroscopic Measurements ◽  
Ic50 Value

Aims and Objective: A series of novel phthalazine derivatives was synthesized with versatile, readily accessible electrophilic and nucleophilic reagents. The newly synthesized compounds were confirmed by the results of spectroscopic measurements. Hence, their potential clinical application investigated in particular for cancer treatment. Materials and Methods: The newly synthesized compounds were characterized by spectroscopic measurements and were tested for their in vitro anticancer activity by MTT assay against human liver cancer cell line. Docking study of all the synthesized compounds was performed within the active site of the enzyme VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2). Results: The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. Docking study showed that the synthesized compounds were fit in the VEGFR-2 active site almost at the same position of sorafenib and vatalanib with comparable docking scores (-15.20 to -8.92 was kcal/mol). Conclusion: we have synthesized a novel series of phthalazine derivatives and evaluated their potential anticancer activity against HEPG2 cell line. The quinazoline derivative 12 emerged as the most potent compound in this study with an IC50 value of 5.4 µM. The SAR and docking studies pointed out that rigidification of the structure resulted in better activity and better binding within the active site of VEGFR-2 as in compounds 3, 5, 6 and 12. These results introduced new phthalazine derivatives having promising activity which could lead to the development of more potent anticancer agents.

Synthesis, Characterization, Anti-proliferative Evaluation, and DNA Flow Cytometry Analysis of Some 2-Thiohydantoin Derivatives

2020 ◽  
Vol 20 (18) ◽  
pp. 1929-1941
Author(s):  
Heba A. Elhady ◽  
Hossa F. Al-Shareef
Keyword(s):  
Anticancer Activity ◽  
Schiff Bases ◽  
Anticancer Agents ◽  
Proliferative Activity ◽  
Cancer Cell Line ◽  
Aromatic Aldehydes ◽  
Pharmaceutical Chemistry ◽  
Dna Flow Cytometry ◽  
Quinazoline Derivative ◽  
Reference Drug

Background and Objective: Due to the well-documented anti-proliferative activity of 2-thiohydantoin incorporated with pyrazole, oxadiazole, quinazoline, urea, β-naphthyl carbamate and Schiff bases, they are noteworthy in pharmaceutical chemistry. Methods: An efficient approach for the synthesis of a novel series of 2-thiohydantoin derivatives incorporated with pyrazole and oxadiazole has proceeded via the reaction of the acyl hydrazide with chalcones and/or triethyl orthoformate. Schiff bases were synthesized by the reaction of the acyl hydrazide with different aromatic aldehydes. Moreover, Curtius rearrangement was applied to the acyl azide to obtain the urea derivative, quinazoline derivative, and carbamate derivative. Results: The synthesized compounds structures were discussed and confirmed depending on their spectral data. The anticancer activity of these heterocyclic compounds was evaluated against the breast cancer cell line (MCF-7), where they showed variable activity. Compound 5d found to have a superior anticancer activity, where it has (IC50 = 2.07 ± 0.13 μg/mL) in comparison with the reference drug doxorubicin that has (IC50 = 2.79 ± 0.07 μg / mL). Then compound 5d subjected to further studies such as cell cycle analysis and apoptosis. Apoptosis was confirmed by the upregulation of Bax, downregulation of Bcl-2, and the increase of the caspase 3/7percentage. Conclusion: Insertion of pyrazole, oxadiazole and, quinazoline moieties with 2-thiohydantoin moiety led to the enhancement of its anti-proliferative activity. Hence they can be used as anticancer agents.

Isolation of New Glycosides from Anemarrhena Asphodeloides Rhizome and Screening of their Anticancer Activity

2019 ◽  
Vol 16 (6) ◽  
pp. 474-477 ◽  
Author(s):  
Pham Van Khang ◽  
Nguyen Thi Hien Lan ◽  
Le Quang Truong ◽  
Mai Thi Minh Chau ◽  
Mai Xuan Truong ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Spectral Data ◽  
Cell Lines ◽  
Cancer Cell ◽  
Spectroscopic Analysis ◽  
2D Nmr ◽  
Ic50 Values ◽  
Nmr Techniques ◽  
Inhibitory Activities ◽  
Anemarrhena Asphodeloides

In this report, two new steroidal glycosides were isolated and determined from n-butanol fraction of A.asphodeloides. The structures were confirmed in comparison with the spectral data of known compounds by using different spectroscopic analysis approaches including 1D & 2D-NMR techniques and HRMS. The anti-proliferation screening against cancer cell lines A549 and HeLa indicated that compound 1 exhibited good inhibitory activities with IC50 values of 0.79 and 0.55 µg/mL, respectively.

Flavon- and Flavonolglycosides from Achillea pannonica Scheele

2001 ◽  
Vol 56 (7-8) ◽  
pp. 521-525 ◽  
Author(s):  
Denata Kasaj ◽  
Liselotte Krenn ◽  
Sonja Prinz ◽  
Antje Hüfner ◽  
Shi Shan Yuc ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
2D Nmr ◽  
Flavonoid Glycosides ◽  
Spectroscopic Methods ◽  
Esi Ms ◽  
Aerial Parts ◽  
Nmr Techniques ◽  
Chemotaxonomic Study ◽  
First Time ◽  
C Nmr

The detailed investigation of a methanolic extract of aerial parts of Achillea pannonica SCHEELE. within a chemotaxonomic study led to the isolation of 6 flavonoid glycosides. Besides rutin, apigenin-7-O-glucopyranoside, luteolin-7-O-glucopyranoside, apigenin-7-O-rutinoside and acacetin-7-O-rutinoside, an unusual flavondiglucoside was isolated. Its structure was established by UV, 1HNMR and 13C NMR spectroscopic methods including 2D-NMR techniques and ESI-MS as luteolin-7,4′-O-β-diglucoside. This substance is reported for the first time in the genus Achillea. Chemotaxonomic aspects are discussed briefly

scholarly journals ISOLASI SENYAWA TURUNAN NAPTOKUINON DARI KULIT BATANG FALOAK (Sterculia quadrifida R.BR) DAN UJI AKTIVITAS ANTIKANKER PADA SEL KANKER PAYUDARA JENIS T47D

2017 ◽  
Vol 5 (1) ◽  
pp. 12 ◽  
Author(s):  
Rollando Rollando ◽  
Rokiy Alfanaar
Keyword(s):  
Breast Cancer ◽  
Anticancer Activity ◽  
Breast Cancer Cells ◽  
2D Nmr ◽  
Isolation Method ◽  
Active Compounds ◽  
Mtt Method ◽  
Activity Test ◽  
Ic50 Value ◽  
Naphthoquinone Derivative

ABSTRAK: Faloak (Sterculia quadrifida R.Br) digunakan secara empiris oleh penduduk Nusa Tenggara Timur untuk mengobati hepatitis, tifus, maag, dan pemulih stamina. Informasi senyawa aktif yang terkandung didalam kulit faloak secara spesifik belum dipublikasi. Penelitian ini bertujuan untuk mengetahui senyawa aktif yang terdapat didalam kulit faloak sebagai antikanker. Ekstraksi menggunakan metode maserasi, isolasi menggunakan metode isolasi bertingkat, elusidasi menggunakan penggabungan informasi dari spektra IR, 1D-NMR, 2D-NMR dan LC-MS, dan uji aktivitas antikanker pada sel kanker payudara T47D menggunakan metode MTT. Hasil isolasi diperoleh isolat turunan senyawa naptokuinon yaitu 2,3-dihydro-6-hydroxy-2-methylenenaphtho[1,2-b]furan-4,5-dione yang aktif sebagai antikanker dengan nilai IC50 pada sel kanker payudara sebesar 9,88 µg/mL dan dengan nilai selektivitas indeks sebesar 30,23.     ABSTRACT: Faloak (Sterculia quadrifida R.Br) is used empirically by residents of East Nusa Tenggara to treat hepatitis, typhoid, ulcers, and stamina restorers. The information of the active compounds contained in the faloak skin is not specifically published. This study aims to determine the active compounds contained in the bark of faloak as anticancer. The extraction was conducted with maceration method followed by a multilevel isolation method. The elucidation was carried out using information of IR spectra, 1D-NMR, 2D-NMR and LC-MS. The anticancer activity test on T47D breast cancer cells was also conducted using MTT method. Based on the results obtained, the active compound is naphthoquinone derivative compound which is 2,3-dihydro-6-hydroxy-2-methylenenaphtho [1,2-b] furan-4,5-dione that has anticancer activity on breast cancer cell (T47D) with IC50 value of 9.88 µg/mL and index selectivity value of 30.23.

scholarly journals (22E,24S)-24-Propylcholest-5en-3α-acetate: A New Steroid from the Stembark Aglaia angustifolia (Miq.) (Meliaceae)

Molbank ◽  
10.3390/m1112 ◽  
2020 ◽  
Vol 2020 (1) ◽  
pp. M1112
Author(s):  
Ricson P. Hutagaol ◽  
Desi Harneti ◽  
Ace T. Hidayat ◽  
Nurlelasari Nurlelasari ◽  
Rani Maharani ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Spectroscopic Data ◽  
Cancer Cell Line ◽  
2D Nmr ◽  
Spectroscopy Analysis ◽  
Weak Activity ◽  
High Resolution Mass Spectroscopy ◽  
Mass Spectroscopy Analysis ◽  
Resolution Mass ◽  
Mcf 7

A new propylcholesterol-type steroid, namely (22E,24S)-24-propylcholest-5en-3α-acetate (1), has been isolated from the stembark of Aglaia angustifolia (Miq.). The structure of 1 was determined on the basis of spectroscopic data including 1D- and 2D-NMR as well as high resolution mass spectroscopy analysis. Compound 1 showed weak activity against the MCF-7 breast cancer cell line.

scholarly journals Synthesis, Molecular Docking and Anticancer Activity of Novel 1,3-Thiazolidin-4-Ones

2020 ◽  
Vol 27 (3) ◽  
pp. 345-352
Author(s):  
Ramesh Sawant ◽  
Jyoti Wadekar ◽  
Rushikesh Ukirde ◽  
Ganesh Barkade
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Lead Compounds ◽  
Growth Inhibitory ◽  
Growth Inhibitory Activity ◽  
Further Development ◽  
Mcf 7 ◽  
Clinical Strategy

Background: Cancer is a major cause of death all over the globe. Controlling cell division byinhibition of mitosis is the most successful clinical strategy for cancer treatment. The developmentof novel anticancer agents is the most important area in medicinal chemistry and drug discoveryresearch. Thiazolidine is the multifunctional nucleus which shows a number of pharmacologicalactivities like anticancer, anti-inflammatory, antioxidant, antibacterial, antifungal, antidiabetic,antihyperlipidemic and antiarthritic. Methods: In a present study series of 2-substituted-3-(1H-benzimidazole-2-yl)-thiazolidin-4-ones were designed, synthesized by the microwave-assisted system, and characterized bymelting point, IR, 1H NMR, and mass spectroscopy. All the newly synthesized compoundswere examined for their in vitro anticancer activity against breast cancer cell line MCF-7 bySulforhodamine B (SRB) assay. Results: The compounds AB-12 (GI50: 28.5 μg/ml) and AB-6 (GI50: 50.7 μg/ml) exhibitedsignificant cell growth inhibitory activity. Conclusion: These results indicate that compound AB-12 and AB-6 as related polo-like kinase1inhibitors compounds could be lead compounds for further development of anticanceragents.

scholarly journals V. NEGUNDO, L. CAMARA AND B. VARIEGATA PLANTS LEAF EXTRACT EXHIBIT CONSIDERABLE IN VITRO ANTIOXIDANT AND ANTICANCER ACTIVITIES

2017 ◽  
Vol 9 (5) ◽  
pp. 227
Author(s):  
Nutan Badgujar ◽  
Kinnari Mistry ◽  
Jagdish Patel
Keyword(s):  
Anticancer Activity ◽  
Methanolic Extract ◽  
Assay Method ◽  
Human Neuroblastoma Cell ◽  
Anticancer Activities ◽  
Human Neuroblastoma ◽  
Antioxidant Power ◽  
Methanolic Extracts ◽  
Ic50 Value

Objective: The study was planned to investigate antioxidant and anticancer activities with the preliminary phytochemical analysis of methanolic extracts of Vitex negundo (V. negundo), Lantana camara (L. camara) and Bauhania variegata (B. variegata) plants leaf extracts.Methods: Phytochemical evaluation was performed for all the extracts, as per the standard methods. In vitro antioxidant activities were performed by using DPPH (2,2-Diphenyl-1-Picrylhydrazyl), ABTS (2, 2'-Azino-Bis-3-Ethylbenzothiazoline-6-Sulfonic Acid) and FRAP (Ferric reducing antioxidant power assay) method and compared with standard antioxidants. The anticancer activity of plant extract was assessed using MTT colorimetric assay.Results: The study of preliminary phytochemical proved the existence of alkaloids, flavonoids and phenolic types of phytochemicals in high amount. Methanolic extract of L. camara shows minimum IC50 value for DPPH assay (48.75±2.34 µg/ml) and FRAP assay (274.66±3.65 µg/ml). In ABTS assay B. variegata extract exhibit minimum IC50 value (60.48±3.01 µg/ml). Lower the IC50 value of extract, higher the effectiveness of the plant. Methanolic extract of all plants methanolic extracts showed anticancer activity against SH-SY-5Y cells (human neuroblastoma cell) but V. negundo was more effective against SH-SY-5Y cells with IC50 value (209 µg/ml) compared to remaining extracts.Conclusion: The current finding accomplished the in vitro activities, so that plant could be a superior source of antioxidant and anticancer drugs. But further in vivo assessment was needed before adding it into the pharma industry.

scholarly journals Triterpenoids from the Bark of Aglaia glabrata and their In vitro Effects on P-388 Murine Leukemia Cells

2019 ◽  
Vol 35 (1) ◽  
pp. 134-139
Author(s):  
Desi Harneti ◽  
Asep Supriadin ◽  
Rani Maharani ◽  
Nurlelasari Nurlelasari ◽  
Tri Mayanti ◽  
...  
Keyword(s):  
Methanolic Extract ◽  
Leukemia Cell ◽  
2D Nmr ◽  
Leukemia Cell Lines ◽  
Ic50 Value ◽  
In Vitro Effects ◽  
Murine Leukemia Cell ◽  
Reported Data ◽  
Murine Leukemia

Four dammarane-type triterpenoids, dammardienon (1), aglaiabbreviatin E (2), dammar-20,25-dien-3b,24-diol (3) and dammar-24-en-3b,20-diol (4) were isolated from methanolic extract of the bark of Aglaia glabrata. The structures of all triterpenoids were elucidated by 1D-, 2D-NMR, and comparison with previously reported data. All triterpenoids were applied into in vitro bioassay against P-388 murine leukemia cell. Dammar-24-en-3b,20-diol (4) has cytotoxic activity with IC50 value of 9.45 mM towards P-388 murine leukemia cell lines.

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